4-(1,1-Dioxo-1,2-thiazolidin-2-yl)benzoic acid → [4-(3-Cyclopropyl-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][4-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl]methanone

HRID 2411552Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 2411552
[O:1]=[S:2]1(=[O:16])[CH2:6][CH2:5][CH2:4][N:3]1[C:7]1[CH:15]=[CH:14][C:10]([C:11]([OH:13])=O)=[CH:9][CH:8]=1.[CH:17]1([C:20]2[C:21]([N:30]3[CH2:35][CH2:34][NH:33][CH2:32][CH2:31]3)=[N:22][CH:23]=[C:24]([C:26]([F:29])([F:28])[F:27])[CH:25]=2)[CH2:19][CH2:18]1>>[CH:17]1([C:20]2[C:21]([N:30]3[CH2:35][CH2:34][N:33]([C:11]([C:10]4[CH:9]=[CH:8][C:7]([N:3]5[CH2:4][CH2:5][CH2:6][S:2]5(=[O:1])=[O:16])=[CH:15][CH:14]=4)=[O:13])[CH2:32][CH2:31]3)=[N:22][CH:23]=[C:24]([C:26]([F:29])([F:27])[F:28])[CH:25]=2)[CH2:18][CH2:19]1

Komponenten

3

Edukt 2

HCID 66250114-(1,1-Dioxo-1,2-thiazolidin-2-yl)benzoic acidHCID 584847721-(3-Cyclopropyl-5-trifluoromethylpyridin-2-yl)piperazine

Produkt 1

HCID 71253108[4-(3-Cyclopropyl-5-trifluoromethylpyridin-2-yl)piperazin-1-yl][4-(1,1-dioxo-1lambda6-isothiazolidin-2-yl)phenyl]methanoneAusbeute 81,2 %

Versuchsvorschrift

Using 4-(1,1-dioxo-1λ6-isothiazolidin-2-yl)benzoic acid (241 mg) described in Preparation Example 16 and 1-(3-cyclopropyl-5-trifluoromethylpyridin-2-yl)piperazine (271 mg) described in Preparation Example 90 and by the reaction and treatment in the same manner as in Example 87, the title compound (401 mg) was obtained.

Aufarbeitung

  1. customdescribed in Preparation Example 90 and by the reaction and treatment in the same manner as in Example 87

Quellen und Nachweise

ORD-Eintrag
ord-740cf95ec00d403b9ad8fc2e36fea111
Quelldatensatz
uspto-grants-2014_08
Patentnummer
US08816079B2

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